Pactimibe sulfate (CS-505) 是一种ACAT1/2双重抑制剂，对于ACAT1的IC50值为 4.9 μM，对于ACAT2的IC50值为 3.0 μM。Pactimibe sulfate (CS-505) 抑制ACAT，其IC50值在肝细胞中是 2.0 μM，在巨噬细胞中是 2.7 μM，在 THP-1 细胞中是 4.7 μM。Pactimibe sulfate (CS-505) 非竞争性抑制oleoyl-CoA，Ki是5.6 μM。此外，Pactimibe sulfate (CS-505) 明显抑制胆固醇酯的形成，IC50是6.7 μM。Pactimibe sulfate (CS-505) 具有抗动脉粥样硬化的潜力，可降低血浆胆固醇的活性。

Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC 50 s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC 50 s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively [1]. Pactimibe sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a K i value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC 50 of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity [2].

Pactimibe sulfate (CS-505) induces moderate ACAT inhibition in monocyte-derived macrophages, leading to the suppression of foam cell formation [2].

Pactimibe sulfate (CS-505; 60 and 200 mg/kg/day; oral gavage; twice a day; 12 weeks) induces an inhibition for ACAT-1 and ACAT-2, causing a reduction of plasma cholesterol but no influence on macrophage- or collagen-positive areas [3]. Animal Model: Male C57BL/6J ApoE / mice aged 8-week-old [3] Dosage: 60 and 200 mg/kg/day Administration: Oral gavage; twice a day; 12 weeks Result: Decreased plasma cholesterol levels by 39% and 74% at the administration of 60 and 200 mg/kg/day.

608510-47-0

C25H42N2O7S

465.65

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years